REVIEW article
Front. Physiol.
Sec. Gastrointestinal Sciences
The role of bile acid-activated receptor TGR5 in inflammation and liver diseases
Provisionally accepted- Chongqing General Hospital, Chongqing, China
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Takeda G-protein-coupled receptor 5 (TGR5), a bile acid receptor, has been recognized as an important signal molecule with roles extending far beyond bile acid homeostasis. Its activation has been shown to ameliorate metabolic disorders and suppress inflammatory responses through diverse mechanisms. Expressed widely in both parenchymal and non-parenchymal cells of the liver, TGR5 plays a central role in hepatic physiology and disease. This review consolidates current evidence on the involvement of TGR5 in various liver pathologies, including metabolic dysfunction-associated steatohepatitis, cholestatic diseases, liver fibrosis, and hepatocellular carcinoma. Additionally, we summarize the regulatory functions of TGR5 in immune cells and inflammatory signaling pathways. We emphasize TGR5 as a promising therapeutic target for a range of chronic liver diseases, given its pivotal role in modulating inflammation and metabolism. Future research should focus on developing tissue-specific TGR5 agonists to enhance therapeutic efficacy and reduce systemic side effects, as well as elucidating its context-dependent dual roles in hepatocarcinogenesis to ensure safe clinical application.
Keywords: Bile acids, Hepatocellular Carcinoma, Inflammation, Liverfibrosis, Metabolic dysfunction-associated fatty liver disease, tgr5
Received: 16 Nov 2025; Accepted: 02 Feb 2026.
Copyright: © 2026 Xiang, Xiang, Wang, Wu, Luo and Zhang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence: Jie Zhang
Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.
